Estrogenic activity of a polyphenolic extract of the leaves of Epimedium brevicornum

Ghent University, Faculty of Pharmaceutical Sciences, Laboratory of Pharmacognosy and Phytochemistry, Harelbekestraat 72, B-9000 Ghent, Belgium.
Fitoterapia (Impact Factor: 2.35). 02/2005; 76(1):35-40. DOI: 10.1016/j.fitote.2004.10.002
Source: PubMed


The estrogenic activity of a polyphenolic extract of the leaves of Epimedium brevicornum and five fractions obtained by solid-phase extraction were investigated using estrogen-responsive bioassays, a yeast cell assay and the Ishikawa Var-I assay. The extract was found to exhibit significant estrogenic activity in both assays. Furthermore, bioassay-guided fractionation led to localisation of the estrogenicity in the relatively non-polar fractions of the polyphenolic extract.

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    • "These phytoestrogen flavonoids have been shown to exert protective effects on bone loss in OVX rats and postmenopausal women [12, 13]. However, it has been demonstrated that Epimedium flavonoids are weak estrogen agonists that act via the ERα and ERβ [14]. Phytoestrogens have the ability to interfere with estrogen action either by interacting directly with the estrogen receptor (ER) or indirectly by modulating endogenous estrogen concentrations [15, 16]. "
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    ABSTRACT: Er-Xian Decoction (EXD), Epimedium herbs (herbs of Epimedium brevicornum Maxim, EBH), and icariin (ICA) have been proven to have estrogen-like and antiosteoporotic activity and are used for the treatment of osteoporosis, menopausal syndrome, and age-associated diseases. The present study found that EXD, EBH, and ICA treatments, emulating estrogen, significantly contributed to bone density and architecture in OVX rats and that EXD is similar to estrogen and exerts a concomitant effect on bone formation and bone resorption at the tissue level, while EBH and ICA produced bone-protective effects mainly by inhibiting bone resorption. Nevertheless, EXD, EBH, and ICA treatments manifested a fewer adverse effects on the uterus, mammary gland, and vagina compared to estrogen administrations. Among the EXD, EBH, and ICA, EXD was found to have superior efficacy and safety profile.
    Evidence-based Complementary and Alternative Medicine 11/2012; 2012(7):241416. DOI:10.1155/2012/241416 · 1.88 Impact Factor
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    • "The hydrolytic activity was assayed by monitoring the formation of p-nitrophenol following enzymatic hydrolysis of PNPPP [20, 27, 28]. This experimental approach has been applied elsewhere for detection of biological activities of some plant extracts towards PNPPP [29]. The pattern of relaxation produced by the extract that mimics the effect of sildenafil coupled with enzyme substrate inhibitory effect of the extract suggested that phosphodiesterase inhibition was the possible mode of action of the extract on CCSM. "
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    Evidence-based Complementary and Alternative Medicine 01/2012; 2012(1741-427X):137386. DOI:10.1155/2012/137386 · 1.88 Impact Factor
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    • "Briefly, shikonin did not demonstrate estrogenic activity, even at high concentra- tions. Estrogenic activity has been assessed intensively among a great deal of substances including phytocompounds, medicines, pesticides and industrial chemicals using various techniques (De Naeyer et al. 2005; Gutendorf and Westendorf 2001; Sookvanichsilp et al. 2008). According to well-elucidated mechanisms of action (Tsai and O'Malley 1994), in vitro methods use more definitive end points and are more sensitive than in vivo methods. "
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